GNE-049 Inhibitor

Name: GNE-049 Inhibitor; MyBioSource
Brand: MyBioSource
SKU: MBS5754908
Availability: InStock
Rating: 5 (10 reviews)

For Research Use Only. Not for use in diagnostic procedures. Catalog #: MBS5754908

GNE-049 is a highly potent and selective inhibitor of CBP (IC50: 1.1nM in TR-FRET assay). GNE-049 also inhibits BRET and BRD4(1) (IC50s: 12nM and 4200nM, respectively). More details

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Product Documentation

Sample Manual Insert View PDF

Testing Data View PDF

Certificate of Analysis (COA) View PDF

QC Report View PDF

Material Safety Data Sheet View PDF

Technical Datasheet View PDF

Protocol View PDF

Product Overview

Online Datasheet in PDF

Product Name

GNE-049, Inhibitor

Full Product Name

GNE-049

Product Gene Name

GNE-049, inhibitor

Form/Format

Solid. Powder

Purity/Purification

98.00%

Preparation and Storage

Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent

Molecular Weight

510.58

Solubility

DMSO: 100mg/mL (195.86mM) Need ultrasonic
(<1mg/ml refers to the product slightly soluble or insoluble)

Formula

C27H32F2N6O2

SMILES

CC(N1CCC(N(C2CCOCC2)N=C3N4CCCC5=C4C=C(C(F)F)C(C6=CN(C)N=C6)=C5)=C3C1)=O

CAS Number

1936421-41-8

Target & IC50

CBP: ic50 1.1nM
BRET: ic50 12nM
BRD41: ic50 4200nM

In Vitro

GNE-049 shows acceptable PK in mouse, rat, dog, and monkey. GNE-049 is further evaluated in a rat single dose (30-250mg/kg QD) toxicokinetic study. GNE-049 is selective for CBP/P300 and, importantly, quite selective (3820-fold) over BRD4(1), which revealed from the Determination of potency versus a selection of bromodomains. Furthermore, at the 250mg/kg dose level, the ratio of the unbound drug concentration in the brain to unbound drug concentration in plasma (Kp,uu) 3 hours post-dose is determined to be 0.43, indicating that GNE-049 is penetrating into the CNS and potentially resulting in the observed toxicity.

Product Categories/Family for GNE-049, inhibitor

Chromatin/Epigenetic; Epigenetic Reader Domain; Epigenetics

Product References and Citations for GNE-049, inhibitor

Romero FA, et al. GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP). J Med Chem. 2017 Nov 22;60(22):9162-9183.
Romero FA, et al. GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP). J Med Chem. 2017 Nov 22;60(22):9162-9183.

Other Notes

Small volumes of GNE-049, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

Searchable Terms for GNE-049 purchase

MBS5754908 is an inhibitor targeting GNE-049.